CFTR Inhibitor-172

A cell-permeable 2-thio-4-thiazolidinone compound that acts as a potent, reversible, rapid, and voltage-independent inhibitor of CFTR (cystic fibrosis transmembrane conductance regulator)-mediated Cl^- transport in human airway cells (K_i ~ 300 nM). It does not prevent elevation of cellular cAMP, nor does it inhibit non-CFTR Cl^- channels, MDR-1, ATP-sensitive K⁺ channels, or a series of other transporters even at concentrations as high as 5 µM. Shown to block cholera toxin-induced intestinal fluid secretion in mice. May be also useful for reducing intestinal fluid loss in other secretory diarrheas. The solid form of this compound (Cat. No. 219670) is also available.

Cell permeable: yes

Primary Target
CFTR ion-channel

Reversible: yes

Packaged under inert gas

A 50 mM (5 mg/244 µL) solution of CFTR Inhibitor-172 (Cat. No. 219670) in DMSO.

Following initial thaw, aliquot and freeze (70°C). Aliquots are stable for up to 3 months at -70°C.

Yang, H., et al. 2003. J. Biol. Chem.278, 35079.
Al-Awqati, Q., et al. 2002. J. Clin. Invest.110, 1599.
Ma, T., et al. 2002. J. Clin. Invest.110, 1651.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Irritant (B)